A PRMT6 inhibitor
EPZ020411 is an inhibitor of protein arginine methyltranferase 6 (PRMT6; IC50 = 10 nM) that less potently targets PRMT1 and PRMT8 (IC50s = 119 and 223 nM, respectively).1 It dose-dependently decreases methylation of the PRMT6 substrate H3R2 in A375 cells transiently expressing PRMT6 (IC50 = 0.637 ?M).1 EPZ020411 shows a moderate clearance rate in rats following intravenous bolus administration, and, following 5 mg/kg subcutaneous dosing, has an unbound blood concentration exceeding the PRMT6 biochemical IC50 value for more than 12 hours.1
1.Mitchell, L.H., Drew, A.E., Ribich, S.A., et al.Aryl pyrazoles as potent inhibitors of arginine methyltransferases: Identification of the first PRMT6 tool compoundACS Med. Chem. Lett.6(6)655-659(2015)
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